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Compound rifaximin nanoemulsion and preparation method thereof

A technology of rifaximin and nanoemulsion, which is applied in the field of medicine, can solve the problems of inconvenient use, low bioavailability, and large dosage for children, and achieve the goals of improving sensory quality, reducing toxic and side effects, and reducing intake Effect

Inactive Publication Date: 2012-08-01
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Rifaximin is insoluble in water and is easily inactivated in the stomach. In practical applications, the dosage is large and frequent, and the dosage for the first dose needs to be doubled.
The clinical dosage form of rifaximin is often capsules and tablets, which have low bioavailability and are inconvenient to use for those with swallowing difficulties or children

Method used

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  • Compound rifaximin nanoemulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] (1) Weigh 30 g of RH-40, 5 g of Tween-80, 6.5 g of absolute ethanol, 0.5 g of polyethylene glycol-400, 12 g of ethyl acetate, 3 g of rifaximin, and trimethoprim lactate Ampyridine 0.75 g, deionized water 42.25 g for later use;

[0055] (2) Mix the surfactant and the co-surfactant as the surfactant phase, then add the oil phase and mix;

[0056] (3) Add rifaximin and mix well;

[0057] (4) Add trimethoprim lactate and mix well;

[0058] (5) Slowly add deionized water at room temperature, and stir while adding deionized water, until a clear, transparent, dark red, low viscosity and good fluidity liquid is formed.

Embodiment 2

[0060] Tween-80 30 g, absolute ethanol 8 g, 1,2-propanediol 2 g, butyl acetate 5 g, rifaximin 1 g, trimethoprim lactate 0.25 g, deionized water 53.75 g.

Embodiment 3

[0062] RH-40 25 g, EL-40 20 g, absolute ethanol 1 g, ethyl acetate 13 g, ethyl oleate 1 g, wheat germ oil 2 g, rifaximin 0.1 g, trimethoprim lactate 0.025 g, 37.875 g of deionized water.

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Abstract

The invention discloses compound rifaximin nanoemulsion, which is prepared from the following raw materials in percentage by mass: 30 to 45 percent of surfactant, 1 to 10 percent of cosurfactant, 1 to 16 percent of oil phase, 0.1 to 5 percent of rifaximin, 0.025 to 1.25 percent of trimethoprim lactate and the balance of deionized water. The sum of the mass percentage of the raw materials is 100 percent. The compound rifaximin nanoemulsion is applied to acute and chronic intestinal infection, diarrhea syndrome, diarrhea caused by intestinal flora change, hepatic encephalopathy and the like, obviously improves the bioavailability and stability of rifaximin, is quick in response, lasting in effect and high in safety, and has a wide market prospect in the field of medicines.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new dosage form of rifaximin with antibacterial effect, in particular to a transparent and stable oil-in-water compound rifaximin nanoemulsion and a preparation method thereof. [0002] Background technique [0003] Rifaximin (English name Rifaximin) is a rifamycin derivative, a semi-synthetic antibiotic, and the first non-aminoglycoside intestinal antibiotic. It has a wide antibacterial spectrum and strong antibacterial effect. Compared with other gastrointestinal antibiotics, it is not easy to be absorbed by the intestinal tract when taken orally. It has extremely low toxic and side effects and has a high concentration in the intestinal tract. Bacteria and anaerobic bacteria have high antibacterial activity. Its mechanism of action is to inhibit the synthesis of bacterial RNA by irreversibly binding to the β-subunit of bacterial DNA-dependent RNA polymerase, and finally to inhibit the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61K31/439A61K9/107A61P31/04A61P1/12
Inventor 欧阳五庆周莹欧阳伸雨
Owner NORTHWEST A & F UNIV
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